2025 Volume 25 Issue 12 Pages 531-537
For poorly soluble compounds, the dissolution process often becomes the rate-limiting step in oral absorption; therefore, improving solubility is crucial for enhancing the bioavailability of such compounds. Transglycosylated compounds are derivatives obtained by enzymatic modification to parent compounds, in which a sugar moiety is added. An interesting feature of these compounds is that the addition of just one sugar molecule to the parent compound can dramatically increase its solubility. Investigation into the mechanism underlying this remarkable enhancement revealed that enzyme-treated compounds form molecular aggregates in aqueous solution, and poorly soluble compounds can be solubilized in that structures. Furthermore, it was found that the structure of these molecular aggregates differs depending on the type of transglycosylated compounds. In this study, we introduce the solubility and oral absorption-enhancing effects of four transglycosylated compounds: transglycosylated hesperidin, transglycosylated rutin, transglycosylated stevia, and transglycosylated naringin.
